Oritax - instructions for use, dose, side effects, contraindications

Cephalosporin antibiotic III generation for parenteral administration. It acts bactericidal (it breaks the synthesis of the cell wall of microorganisms). Has a wide range of action. Resistant to the action of most beta-lactamases. Effects on many strains resistant to ampicillin and other cephalosporins. Cefotaxime is usually sensitive:

Aeromonas hydrophila, Bacillus subtilis, Bordetella pertussis; Borrelia burgdorferi; Moraxclla catarrhalis; Citrobacter diversus *; Citrobacter freundii *; Clostridium perfringens; Corynebacterium diptheriae; Escherichia coli; Enterobacter spp. *; Erysipelothrix insidiosa; Eubacterium spp .; Haemophilus spp. (producing and non-reducing penicillinase strains, including ampicillin-resistant); Klebsiella pneumoniae, Klebsiella oxytoca; Staphylococcus spp. (methicillin-sensitive, including producing and non-reducing penicillinase strains); Morganella morganii; Neisseria gonorrhoea (including producing and non-reducing penicillinase strains); Neisseria meningitidis; Propionibacterium spp .; Proteus mirabilis, Proteus vulgaris; Providencia spp .; Streptococcus spp. (including Streptococcus pneumoniae); Salmonella spp .; Serratia spp. *; Shigella spp .; Veillonella spp .; Yersinia spp. *; Pseudomonas spp. (Besides Pseudoinonas aeruginosa, Pseudomonas cepacia).

* - sensitivity depends on epidemiological data and on the level of resistance in each country.

TO cefotaxime are stable: Acinetobacter baumanii; Bacteroides fragilis; Clostridium difficile; Enterococcus spp .; gram-negative anaerobes; Listeria monocytogenes; Staphylococcus spp. (methicillin-resistant strains); Pseudomonas aeruginosa; Pseudomonas cepacia; Stenotrophomonas maltophilia.

Pharmacokinetics:

After a single intravenous dose of 0.5 g, 1 g and 2 g, the maximum concentration in the blood plasma (C_max) is determined after 5 minutes and is about 40 μg / ml, 102 μg / ml and 215 μg / ml, respectively. After intramuscular injection of the drug in doses of 0.5 g and 1 g of C_max is determined after 30 minutes and is approximately 10 μg / ml and 23 μg / ml, respectively.

Connection with blood plasma proteins - 30 - 50%. Bioavailability is 90 to 95%. Creates therapeutic concentrations in most tissues (myocardium, bones, gall bladder, skin, soft tissues) and fluids (synovial, pericardial, pleural, cerebrospinal fluid, sputum, bile, urine) of the body. The volume of distribution is -0.25-0.39 l / kg.

Half-life (T_1/2) - 1 hour with intravenous administration and 1 - 1.5 hours - with a / m introduction.It is excreted by the kidneys - 20 - 36% unchanged, the rest - in the form of metabolites (12 - 25% - in the form of pharmacologically active deacetylcefotaxime and 20-25% in the form of 2 inactive metabolites - M2 and 1M3, deprived of antimicrobial action). In chronic renal failure (CRF) and in the elderly T_1/2 increases by 2 times. T_1/2 in newborns - 0.75 - 1.5 hours, in preterm infants (body weight less than 1500 g) increases to 4.6 hours; in children with a body weight of more than 1500 g -3.4 hours. With repeated iv administration in doses of 1 g every 6 hours for 14 days cumulation is not observed. Penetrates into breast milk, passes through the placental barrier.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to cefotaxime:

- respiratory tract infections,

- urinary tract infections,

- septicemia,

- bacteremia,

- endocarditis,

- Intra-abdominal infections (including peritonitis),

- infections of the central nervous system (including meningitis (with the exception of listeriosis)),

- infections of the skin and soft tissues,

- infection of bones and joints,

- Lyme disease (borreliosis).

Prevention of infections after surgery on the gastrointestinal tract, urological and obstetric-gynecological operations.

Contraindications:

- Hypersensitivity to cefotaxime and other cephalosporins;

- In case of dissolution of the drug with 1% lidocaine solution: hypersensitivity to lidocaine or other local anesthetic of the amide type; intracardiac blockades without an established pacemaker; severe heart failure; intravenous administration;

- children age up to 2.5 years (for intramuscular route of administration).

Carefully:

Patients with a history of allergy to penicillins (risk of developing cross-allergic reactions); with simultaneous use with aminoglycosides; with renal failure.

Pregnancy and lactation:Pregnancy. Cefotaxime penetrates the placental barrier. Studies conducted on animals did not reveal a teratogenic effect of the drug. However, the safety of the use of cefotaxime in pregnancy in humans has not been determined, so the drug should not be used during pregnancy.

Breastfeeding period. Cefotaxime penetrates into breast milk, so if necessary, the drug should be interrupted breastfeeding.

Dosing and Administration:

Intravenous or intramuscular.

The dose, method and frequency of administration should be determined by the severity of the infection, the sensitivity of the pathogen and the patient's condition. Treatment can be initiated before the results of the sensitivity test are obtained.

Adults and children over 12 years of age with a body weight of 50 kg or more:

For infections of mild to moderate severity - 1 g every 12 h.

The dose may vary depending on the severity of the infection, the sensitivity of the pathogen and the condition of the patient. In severe infections, the dose can be increased to 12 g per day, divided into 3 or 4 injections. In infections caused by Pseudomonas spp., daily dose - should be more than 6 g.

Children up to 12 pet and weighing up to 50 kg

The usual dose is 100-150 mg / kg / day, divided into 2 to 4 injections. In very severe infections, the dose can be increased to 200 mg / kg / day.

Newborns:

50 mg / kg / day, divided into 2-4 injections. In severe infections, a dose of 150-200 mg / kg / day, divided into 2-4 injections.

With gonorrhea:

1 g once intravenously or intramuscularly.

FROM prevention of infections before surgery (30 to 90 min before the start of the operation) 1 g intramuscularly or intravenously.

When performing cesarean section at the time of application of the clips to the umbilical vein, 1 g of the drug is intravenously injected, then after 1 and 6 h, 1 g is intravenous or intramuscularly repeated.

With renal failure:

in cases where creatinine clearance less than 10 ml / min, it is necessary to reduce the dose. After the introduction of the initial single dose, the daily dose should be halved without changing the frequency of administration, i.e. instead of 1 g every 12 hours - 0.5 g every 12 h, instead of 1 g every 8 h- 0.5 g every 8 h, instead of 2 g every 8 h - 1 g every 8 h, etc. A further dose adjustment may be required depending on the course of the infection and the general condition of the patient.

Rules for the preparation of solutions

For intravenous injection as a solvent, water for injection is used (500 mg diluted in 2 ml of solvent, 1 g in 4 ml); with intravenous injection, the solution should be injected for 3 to 5 minutes.

For intravenous infusion 0.9% sodium chloride solution or 5% dextrose solution is used as the solvent (1-2 g is dissolved in 40-100 ml of solvent). Ringer's lactate solution can also be used. The duration of the infusion is 20-60 min.

For intramuscular injection use water for injection or 1% lidocaine solution (500 mg diluted in 2 ml of solvent, 1 g - in 4 ml).

The freshly prepared solution is suitable for use for 12 hours when stored at 25 ° C ± 2 ° C, 60% ± 5% relative humidity, and for 24 hours when stored at 2-8 ° C ± 2 ° C, relative humidity 65% ± 5%, in the dark place.

The pale yellow shade of the solution does not mean a decrease in the activity of the antibiotic.

Side effects:

According to the World Health Organization (WHO), unwanted effects are classified according to their frequency of development as follows: very frequent - more than 10%, frequent - from 1 to 10%, infrequent - from 0.1% to 1%, rare - from 0 , 01 to 0.1%, very rare - less than 0.01%, including single cases.

From the side of the blood and lymphatic system

infrequent: leukopenia, eosinophilia, thrombocytopenia, pancytopenia, bone marrow hematopoiesis deficiency;

frequency is unknown (can not be estimated from available data): granulocytopenia, agranulocytosis, neutropenia, hemolytic anemia.

From the nervous system

infrequent: convulsions;

frequency is unknown (can not be estimated from available data): headache, fatigue, encephalopathy (when given in high doses), dizziness, impaired consciousness, movement disorders.

frequency is unknown (can not be estimated from available data): arrhythmia with rapid introduction through the central venous catheter.

From the digestive system

infrequent: diarrhea, increased activity of "liver" transaminases, increased serum bilirubin concentration;

frequency is unknown (can not be estimated from available data): nausea, vomiting, abdominal pain, pseudomembranous colitis, hepatitis (sometimes with jaundice).

From the skin and subcutaneous tissues

infrequent: skin rash, itching, urticaria;

frequency is unknown (can not be estimated from available data): exfoliative multiform erythema, Stevens-Johnson syndrome. toxic epidermal necrolysis, acute generalized exanthematous pustulosis.

From the genitourinary system

infrequent: decreased renal function (increased urea and creatinine in the blood), acute renal failure;

frequency is unknown (can not be estimated from available data): interstitial nephritis.

From the immune system

infrequent: Jarish-Hexheimer reaction;

frequency is unknown (can not be estimated from available data): anaphylactic

reactions, angioedema, bronchospasm. anaphylactic shock.

Local

very frequent: pain at the injection site (with the / m introduction);

infrequent: inflammatory reactions at the site of administration, including phlebitis / thrombophlebitis.

Other

frequency is unknown (can not be estimated from available data): superinfection, excessive growth of cefotaxime-resistant organisms, systemic reactions to lidocaine.

Laboratory indicators

increase in the activity of "hepatic" enzymes (alanine aminotransferase, aspartate aminotransferase, lactate dehydrogenase, gamma glutamyltransferase, alkaline phosphatase) and / or bilirubin concentrations (these deviations in laboratory indicators (which can also be explained by the presence of infection) rarely exceed the upper limit of the norm by a factor of 2 and indicate a lesion of the liver, manifested by cholestasis and often occurring asymptomatically).

As with the use of other antibiotics, in the treatment of borreliosis during the first days of therapy, the development of the Yarisch-Gerxheimer reaction is possible. There are reports of the occurrence of one or more symptoms after a few weeks of treatment of borreliosis: skin rash, itching, fever, leukopenia, increased activity of "liver" enzymes, shortness of breath, discomfort in the joints.

Overdose:

Symptoms: convulsions, reversible encephalopathy (in the case of the administration of large doses, especially in patients with renal insufficiency), tremor, neuromuscular excitability.

Treatment: symptomatic, there is no specific antidote.

Interaction:

Increases the risk of bleeding when combined with antiaggregants, non-steroidal anti-inflammatory drugs.

The probability of kidney damage increases with simultaneous administration with aminoglycosides, polymyxin B and "loop" diuretics.

Drugs that block tubular secretion, increase plasma concentrations of cefotaxime and slow its elimination. For example, probenecid slows the excretion of cefotaxime and increases its plasma concentration.

Cefotaxime does not lead to the development of disulfiram-like reactions when combined with ethanol.

Compatibility guidelines: cefotaxime should not be mixed with other antibiotics (including aminoglycosides), as in one syringe, and in one infusion solution.

Special instructions:Diarrhea (especially severe and persistent) that developed during treatment and in the first weeks after completion of therapy may be a manifestation of Clostridium difficile associated diarrhea (the most severe form is nonsedembranous colitis).In case of suspicion of pseudomembranous colitis, the use of cefotaxime should be stopped immediately and specific antibacterial therapy (for example, vancomycin or metronidazole). In this condition, preparations that inhibit peristalsis are contraindicated.

Before prescribing the drug, you need to collect an allergic medical history, especially with regard to beta-lactam antibiotics. If the patient develops a hypersensitivity reaction, then the treatment should be stopped.

Disorders of hematopoiesis: during treatment with cefotaxime, leukopenia, neutropenia and, more rarely, bone marrow hematopoiesis, pancytopenia and agranulocytosis may develop.

With a duration of treatment more than 10 days should be monitored the number of blood cells. If the deviations from the norm of these blood parameters should be canceled drug.

As cefotaxime excreted mainly through the kidneys, patients with impaired renal function require monitoring of kidney function, as well as correction of the dosing regimen. Kidney function should be monitored in all cases of combined use of cefotaxime with aminoglycosides, other nephrotoxic drugs,in elderly patients or with renal insufficiency.

The rapid administration of cefotaxime through a central venous catheter can lead to arrhythmia.

When determining glucose in the urine by a non-enzymatic method (for example, by the method of Benedict), false positive results are possible.

When using the drug, a false positive Coombs reaction (direct antiglobulin test) is possible.

When using high doses of beta-lactam antibiotics, including cefotaxime, especially in patients with impaired renal function, the risk of encephalopathy increases.

It is necessary to take into account the sodium content in the Oritax preparation (24.1 mg sodium in the dosage form 0.5 g cfotaxime, 48.2 mg sodium in the dosage form 1 g cefotaxime) when prescribing cefotaxime to patients who need to limit sodium intake.

There is no need for special precautions when destroying an unused preparation.

It is recommended to use glucose oxidase methods to determine the concentration of glucose in the blood, due to the development of false positive results with the use of nonspecific reagents.

Effect on the ability to drive transp. cf. and fur:

The effect of Ortax on the ability to drive vehicles and other activities that require concentration and speed of psychomotor reactions has not been studied.

In the case of the development of such a side effect as dizziness, the ability to concentrate attention and reactions may be impaired. In this case, patients should refrain from driving vehicles and working with mechanisms.

Form release / dosage:

Powder for the preparation of solution for intravenous and intramuscular injection.

Packaging:

For 500 mg and 1000 mg of active ingredient in a vial of transparent glass, sealed with a plug of chlorobutyl rubber, crimped aluminum ring with a safety plastic cap.

Solvent: water for injections (RU No. LP-002377 dated February 18, 2014) to 5 or 10 ml in a vial of colorless neutral glass or from low-density polyethylene with a fault line.

For a dosage of 500 mg:

For 1 bottle with the drug and 1 ampoule of 5 ml or 10 ml with or without solvent, together with instructions for use in a cardboard pack.

For the dosage of 1000 mg:

For 1 vial of the drug and 1 ampoule of 10 ml or 2 ampoules of 5 ml with or without solvent, together with the instructionsapplication in a cardboard box.

For hospitals:

10, 25, 48 or 100 vials with the preparation and, respectively:

for dosage of 500 mg - 10, 25, 48 or 100 ampoules of 5 ml or 10.0 ml with or without solvent, together with instructions for use in an amount equal to the number of bottles, in a cardboard box;

for dosage of 1000 mg - 10. 25, 48 or 100 ampoules of 10.0 ml or 20, 50, 96 or 200 ampoules of 5.0 ml with or without solvent, together with instructions for use in an amount equal to the number of bottles, in a cardboard box .

Storage conditions:In dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001139/10

Date of registration:18.02.2010 / 16.04.2015

Expiration Date:Unlimited

The owner of the registration certificate:JODAS EKSPOIM, LLC JODAS EKSPOIM, LLC Russia

Manufacturer: & nbsp

JODAS EXPOIM, Pvt. Ltd. India

Representation: & nbspJodas Expoim, Open CompanyJodas Expoim, Open Company

Information update date: & nbsp11.06.2017

Illustrated instructions

Instructions

Ortax (Oritax)